“…That other sulfonamides may be assayed by this same procedure is exemplified by the data summarized in Table 2, although a separate standard curve must be constructed for each sulfonamide. Variations in lowest useful concentrations and regression coefficients may reflect differences in solubility, intrinsic antibacterial activities (7,9), degrees of diffusion through the agar medium (4), or susceptibility to sulfonamide anatagonists in the clinical specimens (20,23). These considerations preclude the application of this technique to the assay of body fluids from individuals receiving multisulfonamide dosing.i Typical regressior.…”
Section: Resultsmentioning
confidence: 99%
“…Sulfacytine (l-ethyl-N-sulfanilylcytosine) is a highly soluble, "short acting" sulfonamide (7,9). To study its distribution in normal volunteers, it was important to determine the proportion of active (free) sulfacytine present in blood and urine.…”
A reasonably precise, reproducible, and sensitive microbiological procedure for directly assaying sulfacytine and other sulfonamides as antibacterially active drugs has been developed by appropriately modifying the standard disc-agar diffusion technique. Blood and urine levels as low as 3 m2g/ml may be determined through the use of a strain of Escherichia coli and a chemically defined agar medium devoid of sulfonamide antagonists. Results indicate that this assay method should be a useful adjunct to the Bratton-Marshall colorimetric procedure, by permitting the direct measurement of antibacterially active drug in clinical specimens.
“…That other sulfonamides may be assayed by this same procedure is exemplified by the data summarized in Table 2, although a separate standard curve must be constructed for each sulfonamide. Variations in lowest useful concentrations and regression coefficients may reflect differences in solubility, intrinsic antibacterial activities (7,9), degrees of diffusion through the agar medium (4), or susceptibility to sulfonamide anatagonists in the clinical specimens (20,23). These considerations preclude the application of this technique to the assay of body fluids from individuals receiving multisulfonamide dosing.i Typical regressior.…”
Section: Resultsmentioning
confidence: 99%
“…Sulfacytine (l-ethyl-N-sulfanilylcytosine) is a highly soluble, "short acting" sulfonamide (7,9). To study its distribution in normal volunteers, it was important to determine the proportion of active (free) sulfacytine present in blood and urine.…”
A reasonably precise, reproducible, and sensitive microbiological procedure for directly assaying sulfacytine and other sulfonamides as antibacterially active drugs has been developed by appropriately modifying the standard disc-agar diffusion technique. Blood and urine levels as low as 3 m2g/ml may be determined through the use of a strain of Escherichia coli and a chemically defined agar medium devoid of sulfonamide antagonists. Results indicate that this assay method should be a useful adjunct to the Bratton-Marshall colorimetric procedure, by permitting the direct measurement of antibacterially active drug in clinical specimens.
“…Xanthine sulfonamides 7 − 21 , 23 − 29 , and 37 − 41 are prepared by sulfonating N (1), N (3)-di- n -butylxanthines 5 and 6 with various sulfonyl chlorides using either (a) K 2 CO 3 in acetone at 23 °C or (b) i -Pr 2 NEt in CH 2 Cl 2 at 23 °C. Sulfonamides 31 − 36 were prepared by selectively sulfonating N (3)- n -butylxanthine 30 at N(7) with 3,4-dimethoxybenzenesulfonyl chloride in CH 2 Cl 2 at 23 °C, followed by alkylation at N(3) with alkyl bromides using K 2 CO 3 in DMF at 23 °C (Scheme ). 1 …”
A series of xanthine sulfonamides is presented as a class of calcitonin (CT) inducers - a potentially new method for treating diseases associated with postmenopausal bone loss such as osteoporosis. We have found that certain di-n-butylxanthine sulfonamides 4 upregulate CT transcription in a CT-luciferase reporter gene assay (CT-luci) and increase the production and release of CT in a CT secretion/RIA assay (CTS). In addition, these compounds do not have potent PDE4 inhibitory activity as do the related xanthine methylene ketones such as denbufyllene (2). One compound in particular (9) shows a transcription activation ratio (TAR) of 2.1 in CT-luci, a CTS increase of 3.6-fold, and a PDE4 (phosphodiesterase type IV) IC(50) = 4.1 microM. In addition, this compound showed a statistically significant 47% trabecular bone protection in ovariectomized-induced osteopenia (OVX) rats as determined by assay when administered for 4 weeks at 30 mg/kg/day, i. p. by quantitative computed tomography (QCT). When administered p.o., compound 9 shows 50% trabecular bone protection when administered for 3 weeks at 50 mg/kg/day, i.p. This compared with salmon CT which shows 62% trabecular bone protection when administered at 50 IU/kg/day for 4 weeks.
“…But their narrow safety margin precluded further follow-up studies. Derivatives [35][36][37][38] of 2-(iv-phenacyl)-3-hydrazino-5,5-dimethyl-2-cyclohexenone were active in tests used to characterize antidepressants and were weakly sedative but not anticonvulsant.…”
N-[1-(p-Phenoxyphenyl)ethyl]hexahydro-2H-azepin-2-imine hydrochloride (10) and N-[1-(2-dibenzothienyl)-ethyl]hexahydro-2H-azepin-2-imine hydrochloride (22) were found to inhibit in vitro aggregation of human blood platelets induced by ADP with minimal release of procoagulant platelet factor 3. The compounds were selected from a series of substituted alpha-methylbenzyl and tricyclic arylalkyl lactamimides that were free of hypoglycemic and diuretic effects. Compounds 10 and 22, as well as N-[1-(1-naphthyl)ethyl]hexahydro-2H-azepin-2-imine hydrochloride (I) and N-(2,2-diphenylpentyl)hexahydro-2H-azepin-2-imine hydrochloride (II), were evaluated for effects on ADP-induced platelet aggregation after repeated oral administration to guinea pigs. Compound II (RMI 12,366A) showed in vivo activity in this system 2 h after the last of four daily doses of 100 mg/kg po.
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